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Literature summary for 3.4.23.47 extracted from

  • Tie, Y.; Wang, Y.F.; Boross, P.I.; Chiu, T.Y.; Ghosh, A.K.; Tozser, J.; Louis, J.M.; Harrison, R.W.; Weber, I.T.
    Critical differences in HIV-1 and HIV-2 protease specificity for clinical inhibitors (2012), Protein Sci., 21, 339-350.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor amprenavir, to 1.5 A resolution, and comparison with HIV-1 protease PR1M Human immunodeficiency virus 2

Inhibitors

Inhibitors Comment Organism Structure
amprenavir
-
Human immunodeficiency virus 2
darunavir
-
Human immunodeficiency virus 2
saquinavir
-
Human immunodeficiency virus 2

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.12
-
VSQLYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
0.13
-
KARLMAEALK pH 5.6, 37°C Human immunodeficiency virus 2
0.19
-
VVQNYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
0.24
-
VSQVYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
0.28
-
IPFAAAQQRK pH 5.6, 37°C Human immunodeficiency virus 2
0.4
-
VLQNYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 2
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
IPFAAAQQRK + H2O peptide represents the HIV-2 cleavage site p2/NC Human immunodeficiency virus 2 IPFAA + AQQRK
-
?
KARLMAEALK + H2O peptide represents the HIV-2 cleavage site CA/p2 Human immunodeficiency virus 2 KARLM + AEALK
-
?
VLQNYPIVQ + H2O peptide represents a variation of HIV-1 MA/CA cleavage site Human immunodeficiency virus 2 VLQNY + PIVQ
-
?
VSQLYPIVQ + H2O peptide represents a variation of HIV-1 MA/CA cleavage site Human immunodeficiency virus 2 VSQLY + PIVQ
-
?
VSQVYPIVQ + H2O peptide represents a variation of HIV-1 MA/CA cleavage site Human immunodeficiency virus 2 VSQVY + PIVQ
-
?
VVQNYPIVQ + H2O peptide represents a variation of HIV-1 MA/CA cleavage site Human immunodeficiency virus 2 VVQNY + PIVQ
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.06
-
VLQNYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
0.16
-
VVQNYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
0.3
-
IPFAAAQQRK pH 5.6, 37°C Human immunodeficiency virus 2
0.3
-
KARLMAEALK pH 5.6, 37°C Human immunodeficiency virus 2
0.4
-
VSQLYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
2.6
-
VSQVYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.04
-
darunavir pH 5.6, 37°C Human immunodeficiency virus 2
0.11
-
saquinavir pH 5.6, 37°C Human immunodeficiency virus 2
0.17
-
amprenavir pH 5.6, 37°C Human immunodeficiency virus 2

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.2
-
VLQNYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
0.8
-
VVQNYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
1.1
-
IPFAAAQQRK pH 5.6, 37°C Human immunodeficiency virus 2
2.3
-
KARLMAEALK pH 5.6, 37°C Human immunodeficiency virus 2
3.3
-
VSQLYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
10.8
-
VSQVYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2